PRMT5-IN-56

Overview

PRMT5-IN-56 is a PRMT5 ⋅MTA complex inhibitor with an IC 50 of 0.2 nM, oral activity, and blood-brain barrier penetration. PRMT5-IN-56 inhibits PRMT5 methyltransferase activity in an MTA-cooperative manner, suppresses symmetrical dimethylarginine levels in MTAP-deficient cells. PRMT5-IN-56 suppresses proliferation of MTAP-deleted cancer cells with high selectivity over MTAP-wild type cells. PRMT5-IN-56 induces dose-dependent tumor growth inhibition in subcutaneous xenograft models, inhibits intracranial tumor progression, and prolongs survival in orthotopic brain xenograft models. PRMT5-IN-56 exhibits high intrinsic permeability, good oral bioavailability, and a high brain-to-plasma ratio. PRMT5-IN-56 can be used for the research of MTAP-deleted cancers and glioblastoma.

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Disease Areas > CNS Neoplasm | Products > Disease Areas > Glioma | Products > Disease Areas > Glioblastoma | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Research Areas > Neurological Disease | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy

Product Information

• Catalog No.: HY-184290
• CAS No.: 3062852-59-6
• Molecular Formula: C25H24F3N5O2
• Molecular Weight: 483.49
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source